Organocatalyzed enantioselective Mannich reaction of pyrazoleamides with isatin-derived ketimines

J Org Chem. 2014 May 16;79(10):4332-9. doi: 10.1021/jo500145w. Epub 2014 May 5.

Abstract

The first organocatalytic enantioselective Mannich reaction of pyrazoleamides with isatin-derived N-Boc ketimines has been developed to afford 2-oxindole-based chiral β-amino amides in good yields (84-97%) with excellent diastereo- and enantioselectivities (up to 99:1 dr and >99% ee).